Table 2.
Pharmacokinetic parameters of ponesimod in healthy subjects after administration of single doses of 1, 3, 8, 20 (fasted and fed), 50 and 75 mg ponesimod (n = 6 per dose group)
| Dose (mg) | Cmax (ng ml−1) | tmax (h) | AUC0–∞ (ng h ml−1) | t1/2 (h) |
|---|---|---|---|---|
| 1 | 3.4 (2.8–4.2) | 3.3 (1.5–4.0) | 96.0 (75.9–121) | 21.7 (18.1–26.0) |
| 3 | 13.7 (11.9–15.7) | 2.0 (1.5–2.5) | 405 (323–509) | 30.1 (21.6–41.9) |
| 8 | 27.2 (23.7–31.2) | 3.3 (1.5–6.0) | 913 (751–1110) | 33.4 (28.1–39.7) |
| 20 (fasted) | 71.0 (56.0–90.1) | 2.5 (1.5–4.0) | 2344 (1796–3058) | 27.7 (19.2–39.8) |
| 20 (fed) | 81.2 (65.6–100) | 5.0 (4.0–6.0) | 2837 (2264–3356) | 29.7 (21.5–41.1) |
| 50 | 163 (130–205) | 4.0 (2.5–10.0) | 5266 (3942–7035) | 28.8 (20.3–40.8) |
| 75 | 274 (256–292) | 4.0 (2.5–6.0) | 9153 (7456–11 238) | 31.4 (24.4–40.5) |
Data are expressed as geometric means (and 95% confidence intervals) or, for tmax, the median (and range). Abbreviations are as follows: AUC0–∞, area under the plasma concentration–time curve; Cmax, peak plasma concentration; t1/2, terminal elimination half-life; and tmax, time to maximal concentration.